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GA-017

Cat. No. M21084
GA-017  Structure
Size Price Availability Quantity
5mg USD 265  USD265 In stock
10mg USD 410  USD410 In stock
25mg USD 750  USD750 In stock
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Quality Control & Documentation
Biological Activity

GA-017 is a potent and selective inhibitor of LATS1 and LATS2 (large tumor suppressor kinase 1/2) with IC50 values of 4.10 and 3.92 nM, respectively.GA-017 is a cell proliferation activator.GA-017 promotes YAP/TAZ activation and nuclear translocation.GA-017 promotes cell growth in 3D culture conditions.GA-017 Enhances the formation of mouse intestinal organoid isolates.

Chemical Information
Molecular Weight 343.38
Formula C18H21N3O4
CAS Number 2351906-74-4
Form Solid
Solubility (25°C) DMSO : 20.83 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Ayako Aihara, et al. J Biol Chem. Small molecule LATS kinase inhibitors block the Hippo signaling pathway and promote cell growth under 3D culture conditions

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